activator protein 1

T-5224 is a transcription factor c-Fos AP-1 inhibitor that specifically inhibits the DNA-binding activity of c-Fos c-Jun without affecting other transcription factors.

VVD-130037 is a small molecule activator specifically targeting Kelch-like ECH-associated protein 1 (KEAP1) with potential antitumor activity.VVD-130037 inhibits tumor growth in advanced solid tumors by degrading NRF2.

SR 11302 is an inhibitor of activator protein-1 (AP-1).

CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].

1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human

Birinapant (TL32711) is a synthetic small molecule that is both a peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.

IMM-H007 is a novel lipid-lowering agent, increasing abca1 protein expression

EAAT2 activator 1 (3-[(2-Chloro-6-fluorobenzyl)thio]-6-pyridin-2-ylpyridazine) is a thiopyridazine derivative that has been found to increase EAAT2 protein levels in astrocytes.

SP-100030 is a dual inhibitor of NF-κB and activator protein-1 (AP-1), demonstrating potent inhibition with IC50 values of 50 nM for both. It effectively reduces the production of IL-2, IL-8, and TNF-alpha in Jurkat and other T cell lines. Additionally, SP-100030 has been shown to decrease the severity of murine collagen-induced arthritis (CIA).

Nrf2 activator; inhibits Nrf2 Keap1 interaction. Induces upregulation of Nrf2 pathway downstream gene expression including heme-oxygenase 1. Suppresses LPS-induced TNF-α expression in THP-1 cells.

AMC-04 is a protein response (UPR) activator that initiates the UPR pathway via ROS and p38 MAPK signaling, leading to apoptotic cell death. It is used in cancer research [1].

Euphohelioscopin A, an activator of protein kinase C (PKC), it inhibits proliferation and induces differentiation of the myeloid leukemia cell lines THP-1 and HL-60. Euphohelioscopin A has anti-inflammary activity, it exhibits moderate inhibitory activity

ATUX-1215, a protein phosphatase 2A (PP2A) activator, diminishes the phosphorylation of ERK, p38, JNK, and Akt, as well as decreases the secretion of IL-12p70, GM-CSF, and IL1α in BLM-treated animals, potentially decelerating lung fibrosis progression [1].

Cisd2 agonist 2 (compound 6), with an EC50 of 191 nM, is an orally active activator of Cisd2, a protein whose levels are associated with nonalcoholic fatty liver disease (NAFLD). In vivo studies have demonstrated that Cisd2 agonist 2 exhibits no significant toxicity in heterozygous hepatocyte-specific Cisd2 knockout (Cisd2hKO-het) mice [1].

D-CopA3 is an inhibitor of MDM2 and an activator of the p53 signaling pathway. It exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO with IC50 values of 15-18 μM and induces JNK Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of the cell cycle inhibitor protein p21Cip1 Waf1, enhances mucosal barrier function, and reduces infiltration of inflammatory mediators. It shows anti-inflammatory properties in mouse models of acute enteritis induced by C. difficile toxin A and chronic colitis induced by DSS. Additionally, D-CopA3 demonstrates antitumor activity in a mouse HCT-116 xenograft model.

Teleocidin B-4 serves as a PKC activator, enhancing the accumulation of HIF-1α protein through the PKCα mTORC signaling pathway and upregulating hypoxia-inducible factor 1 (HIF-1) activity. This compound is useful for cancer-related research.

SMAPP1 is an activator of protein phosphatase 1 (PP1). SMAPP1 induces PP1 activity in vitro and activates latent HIV-1 provirus in cultured and primary T cells.

JH-131e-153, a diacylglycerol (DAG)-lactone, serves as a small molecule activator for the C1 domain of Munc13-1, exhibiting an activation hierarchy of WT>I590≈R592A≈W588A. This compound's C1 domain shares sequence and structure homology with protein kinase C (PKC), with an activation preference of PKCα>Munc13-1>PKCε. JH-131e-153 is implicated in the modulation of neuronal processes and holds potential for research in neurodegenerative diseases [1].

γ-AA peptide P6 acts as a potent activator of E6 associated protein (E6AP), facilitating both its self-ubiquitination and the ubiquitination of E6AP substrates in vitro reconstituted reactions. Furthermore, γ-AA peptide P6 amplifies substrate ubiquitination within the cell, thereby expediting their proteasomal degradation [1].

BML-278 is a SIRT1 activator with an EC150 of 1 μM. It increases H3K9 methylation and inhibits H3K9 acetylation in parental and maternal prokaryotes, improving early embryonic development. BML-278 induces cell cycle arrest at the G1 S phase in primary human mesenchymal stromal cells, delaying senescence. It also reduces microtubule protein acetylation in U937 cells and increases mitochondrial density in mouse C2C12 myoblasts.

mSIRK (G-Protein βγ Binding Peptide) is a cell-permeable activator of ERK 1 2 with an EC50 of 2.5-5 μM. It disrupts the interaction between the α and βγ subunits, facilitating α subunit dissociation without inducing nucleotide exchange [1].

Autophagyactivator-1 (Compound B2) is an autophagy activator that induces autophagy by downregulating key members of the HSP70 family and activating the unfolded protein response.

gamma-Linolenic acid (gamolenic acid), is an unsaturated fatty acid synthesized from linoleic acid (LA) by the enzyme delta-6-desaturase. Research on hepatocellular cell lines has shown γ-Linolenic Acid to have induced reactive oxygen species generation including lipid peroxidation, cell growth inhibition, and heme oxygenase-1 production for antioxidant protection against oxidative stress. Further experiments have noted that γ-Linolenic acid inhibits inflammatory responses through inactivation of NFκB and activator protein-1 by suppressed oxidative stress.

TAT (48-57) (TFA) is a cellular permeability peptide derived from hiv-1 transcriptional activator (TAT) protein residue 48-57.